METHODS AND SYSTEMS FOR FORMING BORONIC ACIDS AND INTERMEDIATES THEREOF

PROBLEM TO BE SOLVED: To provide methods and systems for forming boronic acids and intermediates thereof.SOLUTION: A method comprises the steps of: mixing a 1-chloro-2-substituted-3-fluorobenzene starting material with an alkyllithium in a first reactor to form a reaction mixture; and continuously t...

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Hauptverfasser: MARK V M EMONDS, CATHERINE A MENNING, D WAYNE BLAYLOCK
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CATHERINE A MENNING
D WAYNE BLAYLOCK
description PROBLEM TO BE SOLVED: To provide methods and systems for forming boronic acids and intermediates thereof.SOLUTION: A method comprises the steps of: mixing a 1-chloro-2-substituted-3-fluorobenzene starting material with an alkyllithium in a first reactor to form a reaction mixture; and continuously transferring the reaction mixture to a second reactor and then continuously introducing to form a boronate. The boronic acids are formed by treating the boronate with aqueous potassium hydroxide, followed by acidification. Such methods may provide continuous formation of the boronic acids and may reduce an amount of a reactive intermediate present during processing as well as cycle times.SELECTED DRAWING: None 【課題】ボロン酸およびその中間体を生成させるための方法及びシステムの提供。【解決手段】第1の反応器中で1−クロロ−2−置換−3−フルオロベンゼン出発物質をアルキルリチウムと混合して反応混合物を生成させるステップと、前記反応混合物は第2の反応器に連続的に移送され、ホウ酸エステルが連続的に導入されてボロン酸エステルを生成させるステップと、前記ボロン酸エステルを水性水酸化カリウムと処理し、次いで酸性化することによってボロン酸が生成される。このような方法によってボロン酸が連続的に生成され、プロセス中に存在する反応性中間体の量ならびにサイクルタイムを低減することができる。【選択図】なし
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subjects ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
title METHODS AND SYSTEMS FOR FORMING BORONIC ACIDS AND INTERMEDIATES THEREOF
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